Ulixertinib (BVD-523, VRT752271)

Catalog No.S7854

Ulixertinib (BVD-523, VRT752271) Chemical Structure

Molecular Weight(MW): 433.33

Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.

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  • Ulixertinib inhibited the proliferation of SUDHL-10 and Raji cells. (A) The activation of ERK1/2 was analyzed by Western blotting. Ulixertinib (0.1, 0.4 and 1.0 nM) significantly inhibited ERK1/2 activation in a dose-dependent manner compared with control cells. Cell proliferation was measured by the CCK-8 assay. Ulixertinib (0.1, 0.4 and 1.0 nM) significantly inhibited proliferation of SUDHL-10 (B) and Raji cells (C) in a time- and dose-dependent manner compared with control cells.

    Int J Clin Exp Med, 2016, 9(6):10955-10962.. Ulixertinib (BVD-523, VRT752271) purchased from Selleck.

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Choose Selective ERK Inhibitors

Biological Activity

Description Ulixertinib (BVD-523, VRT752271) is a potent and reversible ERK1/ERK2 inhibitor with IC50 of <0.3 nM for ERK2. Phase 1.
Targets
ERK1 [1] ERK2 [1]
<0.3 nM
In vitro

In an A375 melanoma cell line containing a b-RAFV600E mutation, Ulixertinib reduces the levels of phosphorylated ERK2 (pERK) and of the phosphorylation of the downstream kinase RSK (pRSK) with IC50 of 4.1/0.14 μM, respectively. Ulixertinib also inhibits A375 cell proliferation with IC50 of 180 nM. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human A375 cells M3;NVGZ2dmO2aX;uJIF{e2G7 MkHUNkBp M1PCZ2lvcGmkaYTpc44hd2ZiRWLLNU8zKGmwIHj1cYFvKEF|N{WgZ4VtdHNiaHHyZo9zcW6pIFKtVmFHKFZ4MEDFJI12fGGwdDDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiCyaH;zdIhwNVKVSzDs[ZZmdCCjZoTldkAzKGi{czDifUBE\Wyub33pZ5MhSXK{YYnTZ4FvXE1iVmTJJIlu[WerbnegZY5idHm|aYOsJGlEPTB;MD6xOEDPxE1? NEDm[20zPTl5N{m4NS=>
human A375 cells NILNOmtRem:uaX\ldoF1cW:wIHHzd4F6 NVPlOJcyPzJiaB?= Ml7QRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCDM{e1JINmdGy|IHjhdoJwemmwZzDCMXJCTiCYNkCwSUBufXSjboSgZYZ1\XJiN{KgbJJ{KGK7IFPlcIxwdWmlczDBdpJigVOlYX7UUUBXXEliaX3h[4lv\yCjbnHsfZNqeyxiSVO1NF0xNjF6IN88US=> M{PtWlI2QTd5OUix

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Protocol

Kinase Assay:[1]
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ERK2 Rapidfire Mass Spectrometry Inhibition of Catalysis Assay:

MEK U911-activated ERK2 protein is expressed and purified in-house. Enzyme and substrate solutions are made up in assay buffer consisting of 50 mM Tris (pH 7.5), 10 mM MgCl2, 0.1 mM EGTA, 10 mM DTT and 0.01% (v/v) CHAPS. 1.2 nM ERK2 protein is prepared in assay buffer and 10 µL is dispensed into each well of a polypropylene, 384-well plate containing test and reference control compounds. The compound plates had previously been dosed with a 12 point range from 100 µM down to 0.1 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 1%. Following a 20 minute pre-incubation of enzyme and compound at room temperature, 10 µL of substrate solution is added consisting of 16 µM Erktide (IPTTPITTTYFFFK) and 120 µM ATP (measured Km) in assay buffer. The reaction is allowed to progress for 20 minutes at room temperature before being quenched by the addition of 80 µl 1% (v/v) formic acid. The assay plates are then run on the RapidFire Mass Spectrometry platform to measure substrate (unphosphorylated Erktide) and product (phosphorylated Erktide) levels.
Cell Research:[1]
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  • Cell lines: A375 cells
  • Concentrations: ~30 μM
  • Incubation Time: 72 h
  • Method: A375 cells are cultured in cell media composed of DMEM, 10% (v/v) Foetal Calf Serum and 1% (v/v) L-Glutamine. After harvesting, cells are dispensed into black, 384-well Costar plates to give 200 cells per well in a total volume of 40 µL cell media, and are incubated overnight at 37°C, 90% relative humidity and 5% CO2 in a rotating incubator. Test compounds and reference controls are dosed directly into the cell plates, into the inner 308 wells, using a Labcyte Echo 555 acoustic dispenser. The cells are dosed over a 12 point range from 30 µM down to 0.03 nM in order to calculate compound IC50s, with a total DMSO concentration in the assay of 0.3%. The cell plates are then incubated for 72 hours at 37°C. Cells were fixed and stained by the addition of 20 µL 12% formaldehyde in PBS/A (4% final concentration) and 1:2000 dilution of Hoechst 33342, with a 30 minute room temperature incubation, and then washed with PBS/A. A cell count is performed on the stained cell plates using a Cellomics ArrayScanTM VTI imaging platform. A Day 0 cell plate is also fixed, stained and read to generate a cell count baseline for determining compound cytotoxic effects as well as anti-proliferative effects.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (198.46 mM)
Ethanol 15 mg/mL (34.61 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 433.33
Formula

C21H22Cl2N4O2

CAS No. 869886-67-9
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03698994 Recruiting Advanced Malignant Solid Neoplasm|ARAF Gene Mutation|BRAF Gene Mutation|GNA11 Gene Mutation|GNAQ Gene Mutation|HRAS Gene Mutation|KRAS Gene Mutation|MAP2K1 Gene Mutation|MAPK1 Gene Mutation|NF1 Gene Mutation|NRAS Gene Mutation|Recurrent Ependymal Tumor|Recurrent Ewing Sarcoma|Recurrent Glioma|Recurrent Hepatoblastoma|Recurrent Histiocytic and Dendritic Cell Neoplasm|Recurrent Langerhans Cell Histiocytosis|Recurrent Malignant Central Nervous System Neoplasm|Recurrent Malignant Germ Cell Tumor|Recurrent Malignant Solid Neoplasm|Recurrent Medulloblastoma|Recurrent Neuroblastoma|Recurrent Non-Hodgkin Lymphoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Recurrent Rhabdoid Tumor|Recurrent Rhabdomyosarcoma|Recurrent Soft Tissue Sarcoma|Refractory Ependymoma|Refractory Ewing Sarcoma|Refractory Glioma|Refractory Hepatoblastoma|Refractory Histiocytic and Dendritic Cell Neoplasm|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Central Nervous System Neoplasm|Refractory Malignant Germ Cell Tumor|Refractory Malignant Solid Neoplasm|Refractory Medulloblastoma|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Refractory Osteosarcoma|Refractory Peripheral Primitive Neuroectodermal Tumor|Refractory Rhabdoid Tumor|Refractory Rhabdomyosarcoma|Refractory Soft Tissue Sarcoma|Wilms Tumor National Cancer Institute (NCI) October 1 2018 Phase 2
NCT03417739 Recruiting Uveal Melanoma Dana-Farber Cancer Institute|BioMed Valley Discoveries Inc March 26 2018 Phase 2
NCT03454035 Recruiting Tumor Solid|Pancreatic Cancer UNC Lineberger Comprehensive Cancer Center|BioMed Valley Discoveries Inc|Pfizer January 30 2018 Phase 1
NCT03155620 Recruiting Advanced Malignant Solid Neoplasm|Ann Arbor Stage III Childhood Non-Hodgkin Lymphoma|Ann Arbor Stage IV Childhood Non-Hodgkin Lymphoma|Childhood Langerhans Cell Histiocytosis|Histiocytic Sarcoma|Juvenile Xanthogranuloma|Malignant Glioma|Recurrent Central Nervous System Neoplasm|Recurrent Childhood Ependymoma|Recurrent Childhood Malignant Germ Cell Tumor|Recurrent Childhood Medulloblastoma|Recurrent Childhood Non-Hodgkin Lymphoma|Recurrent Childhood Rhabdomyosarcoma|Recurrent Childhood Soft Tissue Sarcoma|Recurrent Ewing Sarcoma|Recurrent Glioma|Recurrent Hepatoblastoma|Recurrent Langerhans Cell Histiocytosis|Recurrent Malignant Solid Neoplasm|Recurrent Neuroblastoma|Recurrent Osteosarcoma|Recurrent Peripheral Primitive Neuroectodermal Tumor|Recurrent Rhabdoid Tumor|Refractory Central Nervous System Neoplasm|Refractory Childhood Malignant Germ Cell Tumor|Refractory Ewing Sarcoma|Refractory Glioma|Refractory Hepatoblastoma|Refractory Langerhans Cell Histiocytosis|Refractory Malignant Solid Neoplasm|Refractory Medulloblastoma|Refractory Neuroblastoma|Refractory Non-Hodgkin Lymphoma|Refractory Osteosarcoma|Refractory Peripheral Primitive Neuroectodermal Tumor|Refractory Rhabdoid Tumor|Refractory Rhabdomyosarcoma|Rhabdoid Tumor|Stage III Osteosarcoma AJCC v7|Stage III Soft Tissue Sarcoma AJCC v7|Stage IV Osteosarcoma AJCC v7|Stage IV Soft Tissue Sarcoma AJCC v7|Stage IVA Osteosarcoma AJCC v7|Stage IVB Osteosarcoma AJCC v7|Wilms Tumor National Cancer Institute (NCI) July 24 2017 Phase 2
NCT02994732 Completed Healthy BioMed Valley Discoveries Inc January 2017 Phase 1
NCT02608229 Recruiting Pancreatic Cancer|Cancer of Pancreas|Cancer of the Pancreas|Pancreas Cancer Washington University School of Medicine|BioMed Valley Discoveries Inc|National Cancer Institute (NCI) June 6 2016 Phase 1

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ERK Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID